Compound preparation for treating Alzheimer's disease and preparation method thereof

A compound technology for Alzheimer's disease, applied in the field of medicine, can solve the problems of clinical application limitations, short half-life, etc., achieve the effects of convenient administration, easy control of conditions, and improvement of compliance

Active Publication Date: 2011-08-17
王义明
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, ligustrazine phosphate has obvious liver first-pass effect after oral administration, and its half-life is short (t1 / 2=2.89h), so it is limited in clinical application.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Preparation of transdermal formulations:

[0033] Oleic acid 0.2g (it is used as oil phase, is the matrix that microemulsion forms), polyoxyethylene ether-40 hydrogenated castor oil 2.4g (it is used as cosurfactant, to promote the formation of microemulsion), ethanol 0.8g ( It is used as a co-surfactant to promote the formation of microemulsion and increase its stability) and eucalyptus oil 0.2g (it is used as a transdermal penetration enhancer to promote and help the drug penetrate into the skin better) and stir and mix After uniformity, add 0.008g of huperzine A, and fully dissolve to obtain a uniform and transparent solution; weigh 1.8g of ligustrazine phosphate, add it to water, dissolve it fully after ultrasonication for 10-15min, slowly add it to the above solution, and keep stirring to mix evenly Finally, the huperzine methyl-ligustrazine phosphate microemulsion was obtained; weighed 112g of polyvinyl alcohol (PVA) (used as the binder of the preparation), added w...

Embodiment 2

[0035] Preparation of transdermal formulations:

[0036] Oleic acid 0.2g (it is used as oil phase, is the matrix that microemulsion forms), polyoxyethylene ether-40 hydrogenated castor oil 2.4g (it is used as cosurfactant, to promote the formation of microemulsion), ethanol 0.8g ( It is used as a co-surfactant to promote the formation of microemulsion and increase its stability) and eucalyptus oil 0.2g (it is used as a transdermal penetration enhancer to promote and help the drug penetrate into the skin better) and stir and mix After uniformity, add huperzine A 0.0096g to fully dissolve to obtain a uniform and transparent solution; weigh 14.41g of ligustrazine phosphate, add it to water, dissolve it fully after ultrasonication for 10-15min, slowly add it to the above solution, and keep stirring to mix evenly Finally, the huperzine methyl-ligustrazine phosphate microemulsion was obtained; weighed 112g of polyvinyl alcohol (PVA) (used as the binder of the preparation), added wat...

Embodiment 3

[0038] Preparation of transdermal formulations:

[0039]Oleic acid 0.2g (it is used as oil phase, is the matrix that microemulsion forms), polyoxyethylene ether-40 hydrogenated castor oil 2.4g (it is used as cosurfactant, to promote the formation of microemulsion), ethanol 0.8g ( It is used as a co-surfactant to promote the formation of microemulsion and increase its stability) and eucalyptus oil 0.2g (it is used as a transdermal penetration enhancer to promote and help the drug penetrate into the skin better) and stir and mix After uniformity, add 0.012g of huperzine A, fully dissolve to obtain a uniform and transparent solution; weigh 0.9g of ligustrazine phosphate, add it to water, dissolve it fully after ultrasonication for 10-15min, slowly add it to the above solution, and keep stirring, mix evenly Finally, the huperzine methyl-ligustrazine phosphate microemulsion was obtained; weighed 112g of polyvinyl alcohol (PVA) (used as the binder of the preparation), added water, s...

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PUM

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Abstract

The invention relates to a compound preparation for treating Alzheimer's disease, which is prepared by combining huperzine A and ligustrazine phosphate according to certain proportion. The compound preparation has reasonable compatibility; all components in the compound preparation have the role of collaboratively protecting the nervous system and can carry out intervention on the pathogenesis of the Alzheimer's disease from multiple targets; and the compound preparation disclosed by the invention has an important clinical application meaning.

Description

technical field [0001] The invention relates to a compound preparation for treating Alzheimer's disease and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Huperzine A is a new alkaloid extracted from Huperzia serrata. It is a potent, reversible and highly selective acetylcholinesterase inhibitor with long-lasting effects and less peripheral cholinergic side effects. The side effects are reversible of. At the same time, huperzine A has high lipid solubility, small molecules, and is easy to pass through the blood-brain barrier. It can selectively act on the central nervous system, and its effect on cholinesterase in the cortex and hippocampus is stronger than other parts of the brain. Effective drug for Alzheimer's disease. At present, there are two dosage forms of huperzine A tablets and capsules on the market. Huperzine A is rapidly and completely absorbed orally, widely distributed in the body, slowly metabolized ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4965A61K9/70A61K9/20A61K9/16A61K9/48A61K9/00A61P25/28A61K31/4748
CPCA61K9/0014A61K31/4965A61K47/44A61K31/4748A61K9/1075A61K31/473A61P25/28A61K2300/00
Inventor 王义明
Owner 王义明
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